Plural Ring Sulfurs In The Five-membered Hetero Ring Patents (Class 548/123)
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Patent number: 8658650Abstract: Compounds useful as allosteric potentiators/positive allosteric modulators of the metabotropic glutamate receptor subtype 4 (mGluR4) and methods of using the compounds.Type: GrantFiled: January 28, 2010Date of Patent: February 25, 2014Inventors: P. Jeffrey Conn, Craig W. Lindsley, Corey R. Hopkins, Charles David Weaver, Colleen M. Niswender, Rocco D. Gogliotti, Darren W. Engers
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Patent number: 8343913Abstract: A method of reducing antifungal drug resistance in which Hsp inhibitors, such as Hsp90 inhibitors, are used.Type: GrantFiled: July 5, 2005Date of Patent: January 1, 2013Assignee: Whitehead Institute for Biomedical ResearchInventors: Leah Cowen, Susan L. Lindquist
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Publication number: 20120277185Abstract: To provide novel carboxamides which exhibit an excellent pesticidal activity as pesticides. Carboxamides represented by the following Formula (I) and use thereof as pesticides and an animal parasite control agent: wherein each substituent is as defined in the specification.Type: ApplicationFiled: July 10, 2010Publication date: November 1, 2012Applicant: BAYER CROPSCIENDE AGInventors: Jun Mihara, Koichi Araki, Takuma Mori, Tetsuya Murata, Yasushi Yoneta, Eiichi Shimojo, Teruyuki Ichihara, Masashi Ataka, Katsuhiko Shibuya, Ulrich Görgens
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Patent number: 8227504Abstract: The present invention discloses and claims a series of substituted N-phenyl-pyrrolidinylmethylpyrrolidine amides of formula (I). Wherein R, R1, R2, R3 and R4 are as described herein. More specifically, the compounds of this invention are modulators of H3 receptors and are, therefore, useful as pharmaceutical agents, especially in the treatment and/or prevention of a variety of diseases modulated by H3 receptors including diseases associated with the central nervous system. Additionally, this invention also discloses methods of preparation of substituted pyrrolidinylmethylpyrrolidine amides and intermediates therefor.Type: GrantFiled: March 15, 2010Date of Patent: July 24, 2012Assignee: SanofiInventors: Werngard Czechtizky, Zhongli Gao, William Joseph Hurst, Lothar Schwink, Siegfried Stengelin
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Publication number: 20110319429Abstract: Compounds useful as allosteric potentiators/positive allosteric modulators of the metabotropic glutamate receptor subtype 4 (mGluR4) and methods of using the compounds.Type: ApplicationFiled: January 28, 2010Publication date: December 29, 2011Inventors: P. Jeffrey Conn, Craig W. Lindsley, Corey R. Hopkins, Charles David Weaver, Colleen M. Niswender, Rocco D. Gogliotti, Darren W. Engers
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Patent number: 8058448Abstract: The present invention relates to processes and reagents for oligonucleotide synthesis and purification. One aspect of the present invention relates to compounds useful for activating phosphoramidites in oligonucleotide synthesis. Another aspect of the present invention relates to a method of preparing oligonucleotides via the phosphoramidite method using an activator of the invention. Another aspect of the present invention relates to sulfur-transfer agents. In a preferred embodiment, the sulfur-transfer agent is a 3-amino-1,2,4-dithiazolidine-5-one. Another aspect of the present invention relates to a method of preparing a phosphorothioate by treating a phosphite with a sulfur-transfer reagent of the invention. In a preferred embodiment, the sulfur-transfer agent is a 3-amino-1,2,4-dithiazolidine-5-one. Another aspect of the present invention relates to compounds that scavenge acrylonitrile produced during the deprotection of phosphate groups bearing ethylnitrile protecting groups.Type: GrantFiled: January 9, 2009Date of Patent: November 15, 2011Assignee: Alnylam Pharmaceuticals, Inc.Inventors: Muthiah Manoharan, Michael E. Jung, Kallanthottathil G. Rajeev, Rajendra K. Pandey, Gang Wang
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Patent number: 8017558Abstract: Novel carboxamides of the formula (I) The present application is further directed toward a plurality of processes for preparing these compounds and their use for controlling unwanted microorganisms, and also novel intermediates and their preparation.Type: GrantFiled: December 5, 2006Date of Patent: September 13, 2011Assignee: Bayer Cropscience AGInventors: Ralf Dunkel, Hans-Ludwig Elbe, Jörg Nico Greul, Herbert Gayer, Bernd-Wieland Krüger, Arnd Voerste, Ulrike Wachendorff-Neumann, Peter Dahmen
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Patent number: 7989635Abstract: Methods for preparing an ammonium salt and a lithium salt of a fluorinated bis-sulfonylimide by a practical and efficient method with a high yield with a small number of steps. Further, a high purity ammonium salt of a fluorinated bis-sulfonylimide useful for the method for producing a lithium salt is provided. A method for producing a purified particulate solid (II) of a salt represented by the formula (1), which comprises suspending a particulate solid (I) of a salt represented by the formula (1) in a solvent comprising an etheric oxygen atom-containing compound, and separating the solvent by filtration: [HNR3]+[Q1-SO2—N—SO2-Q2]???(1) wherein each of R's which may be the same or different, is a hydrogen atom or a C1-10 alkyl group, and each of Q1 and Q2 which are independent of each other, is a monovalent fluoroorganic group, or Q1 and Q2 together form a bivalent fluoroorganic group.Type: GrantFiled: February 4, 2010Date of Patent: August 2, 2011Assignee: Asahi Glass Company, LimitedInventor: Masao Iwaya
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Publication number: 20110137021Abstract: The use of N-formamidino-5-amino-3H-1,2,4-dithiazole-3-thiones, 5-phenyl-3H-1,2,4-dithiazole-3-thiones, and derivatives thereof as novel, efficient sulfur-transfer reagents is disclosed. Sulfur transfer from these reagents to compounds containing a P(III) atom (e.g., triphenylphosphine, 5?-O-DMT-thymidine 2-cyanoethyl-(N,N-diisopropyl)phosphoramidite, and 5?-O-DMT-3?-O-levulinyl dithymidilyl 2-cyanoethyl phosphite), was studied in solution by 31P NMR and HPLC. The sulfur transfer from title compounds was also studied in the solid-phase synthesis of oligonucleotide phosphorothioates by phosphoramidite methods. In this application, the efficiency of the sulfur transfer reaction for 2?-deoxyoligonucleotides was better than 99.5%. The novel sulfurizing agents are synthesized, at low cost, using simple chemical methods.Type: ApplicationFiled: December 1, 2010Publication date: June 9, 2011Inventor: Andrei P. Guzaev
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Patent number: 7951523Abstract: In the liquid immersion lithography process, by simultaneously preventing deterioration of a resist film and deterioration of an immersion liquid employed during liquid immersion lithography which uses various immersion liquids, including water, resistance to post exposure delay of the resist film can be improved without increasing the number of processes, thereby making it possible to form a high resolution resist pattern using liquid immersion lithography. Using an alkaline soluble polymer, a crosslinking agent, and a solvent capable of dissolving them as at least constituent component, a composition is prepared and a protective film is formed on the surface of the resist film to be used, using the composition.Type: GrantFiled: July 29, 2005Date of Patent: May 31, 2011Assignee: Tokyo Ohka Kogyo Co., Ltd.Inventors: Keita Ishizuka, Kotaro Endo, Tomovuki Hiranoa
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Patent number: 7947685Abstract: The present invention is concerned with novel pyrazine 2-carboxyamide derivatives of formula (I) wherein R1, R2 and R3 are as defined in the specification. These compounds are useful for the treatment of CNS disorders.Type: GrantFiled: May 22, 2009Date of Patent: May 24, 2011Assignee: Hoffmann-La Roche Inc.Inventors: Georg Jaeschke, Sabine Kolczewski, Richard Hugh Philip Porter, Eric Vieira
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Patent number: 7923142Abstract: There are provided a novel onium salt and a method for optimizing the interface of a negative electrode by the use of the novel onium salt and/or a conventional onium salt. Such a method is characterized in that an electrolyte comprising novel 2,2,2-trifluoro-N-(trifluoromethanesulfonyl)acetamide•tetraethyl ammonium salt is made to intervene between a negative electrode and a positive electrode in an electrochemical device having the constitution: a negative electrode|an electrolyte|a positive electrode, thereby constructing an electrode structure in the electrochemical device, and applying a voltage between the negative electrode and the positive electrode so as for the negative electrode to have a potential of ?1 V to ?5 V in terms of the potential relative to a reference electrode of I?/I3?, thereby forming a passive-state layer comprising a decomposition product of the above electrolyte or salt on the surface of the above negative electrode.Type: GrantFiled: October 10, 2007Date of Patent: April 12, 2011Assignees: Tokuyama Corporation, National Institute of Advanced Industrial Science and TechnologyInventors: Tomonori Matsunaga, Takeo Kawahara, Hajime Matsumoto
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Patent number: 7910745Abstract: It is intended to provide a labeling precursor compound used for selectively producing radioactive halogen-substituted syn-1-amino-3-cyclobutane-carboxylic acids, and to provide a process for producing a radioactive halogen-substituted syn-1-amino-3-cyclobutane-carboxylic acid using the labeling precursor compound. A labeling precursor is used in which a phthalimide group is used as a protective group for protecting the amino group. The syn-form of the radioactive halogen-substituted 1-amino-3-cyclobutane-carboxylic acid can be selectively produced by labeling the labeling precursor with a radioactive halogen followed by deprotecting.Type: GrantFiled: May 15, 2006Date of Patent: March 22, 2011Assignee: Nihon Medi-Physics Co., Ltd.Inventors: Masahito Toyama, Fumie Kurosaki, Akio Hayashi, Osamu Ito
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Patent number: 7879529Abstract: In the liquid immersion lithography process, by simultaneously preventing deterioration of a resist film and deterioration of an immersion liquid employed during liquid immersion lithography which uses various immersion liquids, including water, resistance to post exposure delay of the resist film can be improved without increasing the number of processes, thereby making it possible to form a high resolution resist pattern using liquid immersion lithography. Furthermore, it is possible to apply a high refractive index liquid immersion medium, used in combination with the high refractive index liquid immersion medium, thus making it possible to further improve pattern accuracy. Using a composition comprising an acrylic resin component having characteristics which have substantially no compatibility with a liquid in which a resist film is immersed, particularly water, and are also soluble in alkaline, a protective film is formed on the surface of a resist film used.Type: GrantFiled: July 29, 2005Date of Patent: February 1, 2011Assignee: Tokyo Ohka Kogyo Co., Ltd.Inventors: Kotaro Endo, Masaaki Yoshida, Keita Ishizuka
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Publication number: 20100256384Abstract: Methods for preparing an ammonium salt and a lithium salt of a fluorinated bis-sulfonylimide by a practical and efficient method with a high yield with a small number of steps. Further, a high purity ammonium salt of a fluorinated bis-sulfonylimide useful for the method for producing a lithium salt is provided. A method for producing a purified particulate solid (II) of a salt represented by the formula (1), which comprises suspending a particulate solid (I) of a salt represented by the formula (1) in a solvent comprising an etheric oxygen atom-containing compound, and separating the solvent by filtration: [HNR3]+[Q1-SO2—N—SO2-Q2]???(1) wherein each of R? s which may be the same or different, is a hydrogen atom or a C1-10 alkyl group, and each of Q1 and Q2 which are independent of each other, is a monovalent fluoroorganic group, or Q1 and Q2 together form a bivalent fluoroorganic group.Type: ApplicationFiled: June 21, 2010Publication date: October 7, 2010Applicant: ASAHI GLASS COMPANY, LIMITEDInventor: Masao IWAYA
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Patent number: 7786293Abstract: The present invention provides a process for the sulfurization of phosphorus-containing compounds. More particularly, the process involves contacting the compound to be sulfurized with a sulfur transfer reagent as defined hereinbefore in a solvent or a mixture of solvents.Type: GrantFiled: June 16, 2006Date of Patent: August 31, 2010Assignee: Novartis AGInventors: Pierre Martin, Francois Jean Charles Natt
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Publication number: 20100137609Abstract: Methods for preparing an ammonium salt and a lithium salt of a fluorinated bis-sulfonylimide by a practical and efficient method with a high yield with a small number of steps. Further, a high purity ammonium salt of a fluorinated bis-sulfonylimide useful for the method for producing a lithium salt is provided. A method for producing a purified particulate solid (II) of a salt represented by the formula (1), which comprises suspending a particulate solid (I) of a salt represented by the formula (1) in a solvent comprising an etheric oxygen atom-containing compound, and separating the solvent by filtration: [HNR3]+[Q1-SO2—N—SO2-Q2]???(1) wherein each of R's which may be the same or different, is a hydrogen atom or a C1-10 alkyl group, and each of Q1 and Q2 which are independent of each other, is a monovalent fluoroorganic group, or Q1 and Q2 together form a bivalent fluoroorganic group.Type: ApplicationFiled: February 4, 2010Publication date: June 3, 2010Applicant: ASAHI GLASS COMPANY, LIMITEDInventor: Masao IWAYA
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Patent number: 7723528Abstract: The use of N-formamidino-5-amino-3H-1,2,4-dithiazole-3-thiones as novel, efficient sulfur-transfer reagents is disclosed. The sulfur transfer from these reagents to compounds containing P(III) atom, triphenylphosphine, 5?-O-DMT-thymidine 2-cyanoethyl-(N,N-diisopropyl)phosphoramidite, and 5?-O-DMT-3?-O-levulinyl dithymidilyl 2-cyanoethyl phosphite, was studied in solution by 31P NMR and HPLC. The sulfur transfer from title compounds was also studied in the solid-phase synthesis of oligonucleotide phosphorothioates by phosphoramidite methods. In this application, the efficiency of the sulfur transfer reaction for 2?-deoxyoligonucleotides was better than 99.5%. The novel sulfurizing agents are synthesized, at low cost, using simple chemical methods.Type: GrantFiled: June 5, 2008Date of Patent: May 25, 2010Assignee: AM Chemicals LLCInventor: Andrei P. Guzaev
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Patent number: 7678789Abstract: The present invention relates to 5-imino-5H-[1,2,4]-dithiazol-3-yl-amine and [1,2,4]-dithiazolidine-3,5-diylidene-diamine derivatives as inducers of gluthathione-S-transferase (GST) and NADPH quinone oxidoreductase (NQO), to methods for the preparation of these compounds and to novel intermediates useful for the synthesis of said [1,2,4]-dithiazoli(di)ne derivatives. The invention also relates to the use of a compound disclosed herein for the treatment of adverse conditions associated with cytotoxicity in general and apoptosis in particular. The invention relates to compounds of the general formula (I): wherein wherein the symbols have the meanings given in the specification.Type: GrantFiled: February 9, 2006Date of Patent: March 16, 2010Assignee: Solvay Pharmaceuticals B.V.Inventors: Roelof W. Feenstra, Hiskias G. Keizer, Maria L. Pras-Raves, Bernard J Van Vliet, Gustaaf J. M. Van Scharrenburg
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Publication number: 20090306358Abstract: The use of N-formamidino-5-amino-3H-1,2,4-dithiazole-3-thiones as novel, efficient sulfur-transfer reagents is disclosed. The sulfur transfer from these reagents to compounds containing P(III) atom, triphenylphosphine, 5?-O-DMT-thymidine 2-cyanoethyl-(N,N-diisopropyl)phosphoramidite, and 5?-O-DMT-3?-O-levulinyl dithymidilyl 2-cyanoethyl phosphite, was studied in solution by 31P NMR and HPLC. The sulfur transfer from title compounds was also studied in the solid-phase synthesis of oligonucleotide phosphorothioates by phosphoramidite methods. In this application, the efficiency of the sulfur transfer reaction for 2?-deoxyoligonucleotides was better than 99.5%. The novel sulfurizing agents are synthesized, at low cost, using simple chemical methods.Type: ApplicationFiled: June 5, 2008Publication date: December 10, 2009Inventor: Andrei P. Guzaev
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Patent number: 7612059Abstract: N-[1-oxo-(optionally 2-aza)-2-alkyl-3-(carboxyl or thiol or hydroxyaminocarbonyl or N-hydroxyformamido)-propyl]-(aryl or heteroaryl)-azacyclo4-7alkanes or thiazacyclo4-7alkanes, salts or prodrugs thereof have interesting properties, e.g., in the treatment or prevention of disorders amenable to treatment by PDF inhibitors, such as treatment of bacterial infections.Type: GrantFiled: June 13, 2005Date of Patent: November 3, 2009Assignee: Vicuron Pharmaceuticals, Inc.Inventors: Jeffrey Jacobs, Rakesh K Patel, Jason G Lewis, Dinesh V Patel, Zhengyu Yuan
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Patent number: 7579465Abstract: This invention relates to compounds of formula I their salts, and pharmaceutically acceptable derivatives thereof, pharmaceutical compositions comprising these compounds and their use in the treatment of picornavirus infections in mammals, as well as novel intermediates useful in the preparation of the compounds of formula I.Type: GrantFiled: November 13, 2006Date of Patent: August 25, 2009Assignee: Biota Scientific Managment Pty. Ltd.Inventors: Keith Watson, Guy Krippner, Pauline Stanislawski, Darryl McConnell
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Publication number: 20090187027Abstract: The present invention relates to processes and reagents for oligonucleotide synthesis and purification. One aspect of the present invention relates to compounds useful for activating phosphoramidites in oligonucleotide synthesis. Another aspect of the present invention relates to a method of preparing oligonucleotides via the phosphoramidite method using an activator of the invention. Another aspect of the present invention relates to sulfur-transfer agents. In a preferred embodiment, the sulfur-transfer agent is a 3-amino-1,2,4-dithiazolidine-5-one. Another aspect of the present invention relates to a method of preparing a phosphorothioate by treating a phosphite with a sulfur-transfer reagent of the invention. In a preferred embodiment, the sulfur-transfer agent is a 3-amino-1,2,4-dithiazolidine-5-one. Another aspect of the present invention relates to compounds that scavenge acrylonitrile produced during the deprotection of phosphate groups bearing ethylnitrile protecting groups.Type: ApplicationFiled: January 9, 2009Publication date: July 23, 2009Applicant: ALNYLAM PHARMACEUTICALS, INC.Inventors: Muthiah MANOHARAN, Michael E. JUNG, Kallanthottathil G. RAJEEV, Rajendra K. PANDEY, Gang WANG
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Patent number: 7553964Abstract: Compounds of formula (I) are useful in treating conditions or disorders prevented by or ameliorated by histamine-3 receptor ligands. Also disclosed are pharmaceutical compositions comprising the histamine-3 receptor ligands, methods for using such compounds and compositions, and a process for preparing compounds within the scope of formula (I).Type: GrantFiled: June 1, 2006Date of Patent: June 30, 2009Assignee: Abbott LaboratoriesInventors: Huaqing Liu, Kathryn J. Hancock, legal representative, Marlon D. Cowart, Arthur A. Hancock
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Patent number: 7348017Abstract: A dithiazole compound or a salt thereof is disclosed. The compound inhibits matrix metalloprotease (MMPs) activity and can be used in pharmaceutical and cosmetic compositions for the treatment of skin conditions.Type: GrantFiled: August 28, 2002Date of Patent: March 25, 2008Assignee: Shiseido Co., Ltd.Inventors: Takuya Hiruma, Koji Kobayashi, Shinji Inomata
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Patent number: 7297797Abstract: The invention relates to novel ?1-pyrrolines of the formula (I) in which R1, R2, R3, R4, A1, A2, R5, R6, R7, R8, R9 and Q are as defined in the disclosure, to a process for preparing these compounds and to their use for controlling pests.Type: GrantFiled: September 8, 2003Date of Patent: November 20, 2007Assignee: Bayer CropScience AGInventors: Johannes Rudolf Jansen, Udo Kraatz, Hubertus Stakemeier, Thomas Seitz, Fritz Maurer, Martin Füsslein, Bernd Alig, Christian Funke, Werner Hallenbach, Jörg Konze, Udo Beckmann, Ulrich Görgens
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Patent number: 7198651Abstract: The present invention relates to a method to achieve a reversible change of the colour of hair dyed with an azo dye wherein the change of the colour can be effected by, for example, the salonist or the consumer in a simple manner. The colour of the hair thus dyed may be changed simply by treating the dyed hair with an acid treatment composition at any time after the first dyeing treatment. If desired by the consumer, the colour may be returned to substantially the original post dye colour by treating the hair further with an alkaline treatment composition.Type: GrantFiled: November 26, 2004Date of Patent: April 3, 2007Assignees: Kao Corporation, Fuji Photo Film Co., Ltd.Inventors: Dominic Pratt, Masayoshi Nojiri, Toshio Kawagishi
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Patent number: 7105556Abstract: Compounds are provided which have the structure wherein Q is C or N, X1 is C or N, and R1, R2, R2a, R2b, R2c, R3, Y, A, m, n, X2, X3 and X4 are as defined herein, which compounds are useful as antidiabetic, hypolipidemic, and antiobesity agents.Type: GrantFiled: May 22, 2002Date of Patent: September 12, 2006Assignee: Bristol-Myers Squibb CompanyInventors: Peter T. Cheng, Yoon Jeon, Wei Wang
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Patent number: 7098325Abstract: The invention relates to a process for the sulfurization of phosphorus-containing compounds which comprises contacting the phosphorus compound to be sulfurized with a sulfur transfer reagent of formula (I) wherein R1 is aryl which can be substituted by halo, (C1–C6) alkyl or (C1-C6) alkoxy, and R2 is (C1–C6) alkyl, which could also form a cyclic ring together with R1, in a solvent or a mixture of solvents.Type: GrantFiled: October 7, 2002Date of Patent: August 29, 2006Inventors: Pierre Martin, Francois J Natt
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Patent number: 7087621Abstract: The present invention provides compounds of formula I or a pharmaceutically acceptable salt, solvate, prodrug or isomer thereof and compounds of the formula or a pharmaceutically acceptable salt, solvate, prodrug or isomer thereof. The compounds of the invention inhibit tyrosine kinase activity of growth factor receptors such as HER1, HER2 and HER4 thereby making them useful as antiproliferative agents. The compounds are also useful for the treatment of other diseases associated with signal transduction pathways operating through growth factor receptors.Type: GrantFiled: September 1, 2004Date of Patent: August 8, 2006Assignee: Bristol-Myers Squibb CompanyInventors: Xiaopeng Sang, Xuhua Karen Du, John F. Kadow
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Patent number: 6987104Abstract: N-[1-oxo-(optionally 2-aza)-2-alkyl-3-(carboxyl or thiol or hydroxyaminocarbonyl or N-hydroxyformamido)-propyl]-(aryl or heteroaryl)-azacyclo4-7alkanes or thiazacyclo4-7alkanes, salts or prodrugs thereof have interesting properties, e.g., in the treatment or prevention of disorders amenable to treatment by PDF inhibitors, such as treatment of bacterial infections.Type: GrantFiled: June 14, 2002Date of Patent: January 17, 2006Assignee: Vicuron Pharmaceuticals Inc.Inventors: Jeffrey Jacobs, Rakesh K. Jain, Jason G. Lewis, Dinesh V. Patel, Zhengyu Yuan
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Patent number: 6927215Abstract: The present invention relates to novel heterocyclic fluoroalkenyl thioethers of the formula (I) in which X represents hydrogen, halogen or alkyl, m represents integers from 2 to 10, n represents 0, 1 or 2. y represents unsubstituted or substituted methylene and p represents 1, 2 or 3, and to processes for their preparation and to their use as pesticides.Type: GrantFiled: June 29, 2001Date of Patent: August 9, 2005Assignee: Bayer Cropscience AGInventors: Udo Kraatz, Bernd Gallenkamp, Heiko Rieck, Albrecht Marhold, Peter Wolfrum, Wolfram Andersch, Christoph Erdelen, Peter Lösel, Andreas Turberg, Olaf Hansen, Achim Harder
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Patent number: 6872833Abstract: The present invention relates to compounds of the general formula I wherein R1, R2, R?, R?, n, m and o are defined herein, or a pharmaceutically acceptable salt thereof. It has been found that the compounds of general formula I are adenosine receptor ligands with a good affinity to the A2A-receptor and a high selectivity to the A1- and A3 receptors. These compounds have useful pharmacological activities.Type: GrantFiled: March 30, 2004Date of Patent: March 29, 2005Assignee: Hoffmann-La Roche Inc.Inventors: Alexander Flohr, Roger David Norcross
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Patent number: 6863698Abstract: A method for coloring Keratin-containing fibers which comprises applying a composition containing a compound of formula A—CH?B—CH?A???(I).Type: GrantFiled: June 24, 2002Date of Patent: March 8, 2005Assignee: Henkel Kommanditgesellschaft auf AktienInventors: Horst Hoeffkes, David Rose, Bernd Meinigke
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Publication number: 20040236111Abstract: A dithiazole compound or a salt thereof expressed by formula (I): 1Type: ApplicationFiled: February 23, 2004Publication date: November 25, 2004Inventors: Takuya Hiruma, Koji Kobayashi, Shinji Inomata
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Publication number: 20040138470Abstract: Novel chiral diphosphines (R) or (S), and their use as optically active ligand for preparing diphosphino-metallic complexes, and the diphosphino-metallic complexes containing said chiral diphosphines (R) or (S), and the use of the diphosphino-metallic complexes as catalyst in asymmetric catalysis of unsaturated compounds bearing functional groups.Type: ApplicationFiled: November 20, 2003Publication date: July 15, 2004Inventors: Jean-Pierre Genet, Angela Marinetti, Guillaume Michaud, Michel Bulliard
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Publication number: 20040127525Abstract: The present invention relates to novel heterocyclic fluoroalkenyl thioethers of the formula (I) 1Type: ApplicationFiled: January 30, 2004Publication date: July 1, 2004Inventors: Udo Kraatz, Bernd Gallenkamp, Heiko Rieck, Albrecht Marhold, Peter Wolfrum, Wolfram andersch, Christoph Erdelen, Peter Losel, Andreas Turberg, Olaf Hansen, Achim Harder
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Patent number: 6610707Abstract: Compounds of the formula: wherein R1, Y, W, A and R2 are as defined above are inhibitors of rotamase enzymes in particular FKBP-12 and FKBP-52. The compounds therefore moderate neuronal regeneration and outgrowth and can be used for treating neurological disorders arising from neurodegenerative diseases and nerve damage.Type: GrantFiled: September 1, 1999Date of Patent: August 26, 2003Assignee: Pfizer Inc.Inventors: David John Bull, Robert John Maguire, Michael John Palmer, Martin James Wythes
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Patent number: 6608175Abstract: Certain substituted oxadiazole, thiadiazole and triazole peptoids which are useful as inhibitors of serine proteases, are prepared in various embodiments using Grignard reagents and alkyllithium reagents and various aldehydes to make oxadiazole, thiadiazole and triazole peptoid alcohols, which are then oxidized to the desired keto products.Type: GrantFiled: November 16, 2001Date of Patent: August 19, 2003Assignee: Cortech, Inc.Inventors: Albert Gyorkos, Lyle W. Spruce
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Patent number: 6589914Abstract: The dihalopropene compounds of the general formula (I) have excellent insecticidal/acaricidal activity, so that they are satisfactorily effective for the control of noxious insects, mites and ticks.Type: GrantFiled: March 4, 2002Date of Patent: July 8, 2003Assignee: Sumitomo Chemical Company, LimitedInventors: Noriyasu Sakamoto, Sanshiro Matsuo, Masaya Suzuki, Taro Hirose, Kazunori Tsushima, Kimitoshi Umeda
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Patent number: 6583289Abstract: The present invention provides a new class of materials effective as curatives for anaerobic adhesive compositions. The addition of these materials into anaerobic adhesives as a replacement for conventional curatives, such as APH, surprisingly provides at least comparable cure speeds and physical properties for the reaction products formed therefrom.Type: GrantFiled: June 26, 2001Date of Patent: June 24, 2003Assignee: Loctite (R&D) LimitedInventors: Ciaran B. McArdle, Rory B. Barnes
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Publication number: 20030097003Abstract: An electron accepting monomer having the formula: 1Type: ApplicationFiled: October 28, 2002Publication date: May 22, 2003Inventors: Geoffrey A. Lindsay, Richard A. Hollins, Mathew C. Davis, Andrew P. Chafin
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Patent number: 6531496Abstract: The invention relates to new O-aryldithiazole dioxides, to two processes for their preparation, and to their use as pesticides in crop protection and in the protection of materials.Type: GrantFiled: January 22, 2002Date of Patent: March 11, 2003Assignee: Bayer AktiengesellschaftInventors: Hermann Uhr, Christiane Boie, Heiko Rieck, Bernd-Wieland Krüger, Ulrich Heinemann, Robert Markert, Martin Vaupel, Martin Kugler, Klaus Stenzel, Ulrike Wachendorff-Neumann, Astrid Mauler-Machnik, Karl-Heinz Kuck, Peter Lösel, Shinichi Narabu
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Patent number: 6525086Abstract: The present invention relates to compounds of formula (I) wherein R1, R2, R3, R4, R5, R6, R7, R8, A, X, T, Q, Z, U, Y, Ar, p and n are as defined in the specification. These compounds are useful in the treatment and/or prevention of conditions mediated by nuclear receptors, in particular the Peroxisome Proliferator-Activated Receptors (PPAR).Type: GrantFiled: March 14, 2001Date of Patent: February 25, 2003Assignee: Novo Nordisk A/SInventors: Lone Jeppesen, Paul Stanley Bury, Per Sauerberg
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Publication number: 20030004193Abstract: 1-Heterocycle substituted diarylamines, methods of making and using them, and compositions containing them.Type: ApplicationFiled: July 23, 2002Publication date: January 2, 2003Inventors: Stephen Douglas Barrett, Alexander James Bridges, Haile Tecle, Lu-Yan Zhang
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Patent number: 6417209Abstract: This invention relates to neurotrophic, low molecular weight, small molecule heterocyclic ketone and thioester compounds, compositions containing the same, and the use of such compounds for treating neurological disorders, including physically damaged nerves and neurodegenerative diseases.Type: GrantFiled: December 11, 2000Date of Patent: July 9, 2002Assignee: GPI Nil Holdings, Inc.Inventors: Gregory S. Hamilton, Jia-He Li
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Publication number: 20020052510Abstract: This invention relates to novel N-linked sulfonamides of N-heterocyclic carboxylic acid and carboxylic acid isosteres, their preparation, and use for treating neurological disorders including physically damaged nerves and neurodegenerative diseases, and for treating alopecia and promoting hair growth.Type: ApplicationFiled: December 3, 1998Publication date: May 2, 2002Inventors: GREGORY S. HAMILTON, MARK H. NORMAN, YONG-QIAN WU
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Patent number: 6331537Abstract: This invention relates to novel N-heteorocyclic carboxylic acids and carboxylic acid isosteres, their preparation and use for treating neurological disorders including physically damaged nerves and neurodengenerative diseases, for treating alopecia and promoting hair growth, for treating vision disorders and/or improving vision, and for treating memory impairment and/or enhancing memory performance by administering such compounds.Type: GrantFiled: December 2, 1999Date of Patent: December 18, 2001Assignee: GPI Nil Holdings, Inc.Inventors: Gregory S. Hamilton, Mark H. Norman, Yong-Qian Wu
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Patent number: 6316476Abstract: The invention is drawn to novel antibiotics, XENORXIDES of formula shown below, wherein R1, R2=hydrogen, substituted or unsubstituted alkyl, cycloalkyl, acyl, aryl, aralkyl, or heterocyclyl group; R3=hydrogen, alkyl cycloalkyl, aralkyl or aryl group, produced by bacterial symbiont Xenorhabdus bovienii and/or other Xenorhabdus species, and/or by oxidation of the corresponding dithiolopyrrolone derivatives with oxygen and Xenorhabdus species, and/or its cell-free filtrate, the additional salts thereof, the compositions thereof and their use as medicaments and/or agrochemicals, particularly in the treatment of infectious diseases involving microorganisms susceptible to them, including drug-resistant Staphylococcus.Type: GrantFiled: July 23, 1996Date of Patent: November 13, 2001Assignee: Welichem Biotech Inc.Inventors: John M. Webster, Jianxiong Li, Genhui Chen
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Patent number: 6313164Abstract: Compounds of the formula (I): wherein one of m and n is 0, and the other is 0, 1 or 2; k is 0 or 1 to 12; R1 is hydrogen, a substituent which is an aryl or a heterocyclic, or an optionally substituted alkyl group; A is a single bond, an oxygen atom, a carbonyl group or a group of the formula —N(R2)CO—, —N(R2)CS—, —N(R2)SO2—, —CON(R2)N(R3)CO—, —CON(R2)CO—, —CON(R2)CS—, —CON(R2)SO2—, —O—CO—, —ON(R2)CO—, —ON(R2)SO2—, —O—CON(R2)N(R3)CO—, —O—CON(R2)CO—, —O—CON(R2)SO2—, —CO—O—, —CO—CO—, —CO—CON(R2)N(R3)CO—, —CO—CON(R2)CO—, —CO—CON(R2)SO2—, —N(R2)O—, —N(R2)COCO—, —N(R2)N(R3)CO—, —N(R2)N(R3)SO2—, —N(R2)CON(R3)N(R4)CO—, —N(R2)CON(R3)CO—, —N(R2)CON(R3)SO2&mdasType: GrantFiled: July 15, 1999Date of Patent: November 6, 2001Assignee: Sankyo Company, LimitedInventors: Takashi Fujita, Tomihisa Yokoyama